Lipase inhibiting composition

Abstract

Pharmaceutical compositions that contain a lipase inhibitor having a melting point ≧37° C., a sucrose fatty acid ester wherein the sucrose fatty acid ester is a mono-, di-, tri- or tetra-ester, and optionally one or more pharmaceutically acceptable excipients, are useful for treatment of obesity.

What is claimed is: 
     
         1 . A pharmaceutical composition comprising
 (i) orlistat;   (ii) a sucrose fatty acid ester or a mixture of sucrose fatty acid esters, wherein the sucrose fatty acid ester comprises a sucrose moiety and at least one to four fatty acid moieties, and wherein the fatty acid moiety in the sucrose fatty acid ester or mixture of sucrose fatty acid esters is selected from the group consisting of a C12-C18 saturated fatty acid; and   wherein the sucrose fatty acid ester or a mixture of sucrose fatty acid esters have an HLB value of about 16;   (iii) one or more pharmaceutically acceptable excipients.   
     
     
         2 . The composition according to  claim 1 , wherein the composition comprises 20 to 60 mg orlistat. 
     
     
         3 . The composition according to  claim 1 , wherein the sucrose fatty acid ester or mixture of sucrose fatty acid esters is selected from sucrose palmitate, sucrose stearate, sucrose myristate or sucrose laurate. 
     
     
         4 . The composition according to  claim 1 , wherein 0.05 mg to 20 mg sucrose fatty acid ester or mixture of sucrose fatty acid esters is used per 1 mg orlistat. 
     
     
         5 . The composition according to  claim 1 , wherein the sucrose fatty acid ester contains at least two fatty acid moieties. 
     
     
         6 . The composition according to  claim 5  wherein the two fatty acid moieties are the same or different. 
     
     
         7 . The composition according to  claim 6  wherein the two fatty acid moieties are the same. 
     
     
         8 . The composition according to  claim 1 , wherein the sucrose moiety in the sucrose fatty acid ester or mixture of sucrose fatty acid esters is about 80% mono esterified. 
     
     
         9 . The composition according to  claim 1  wherein in the mixture of sucrose fatty acid esters the most prevalent sucrose fatty acid ester in said mixture is a mono ester. 
     
     
         10 . The composition according to  claim 1 , wherein the at least one fatty acid moiety in the sucrose fatty acid ester is palmitic acid. 
     
     
         11 . The composition according to  claim 1 , wherein the at least one fatty acid moiety in the sucrose fatty acid ester is lauric acid. 
     
     
         12 . The composition according to  claim 1 , wherein the at least one fatty acid moiety in the sucrose fatty acid ester is myristic acid. 
     
     
         13 . The composition according to  claim 1 , wherein the at least one fatty acid moiety in the sucrose fatty acid ester is stearic acid. 
     
     
         14 . The composition according to  claim 1 , wherein the composition comprises one or more pharmaceutically acceptable excipients selected from the group consisting of mannitol, lactose, HPMC, talcum, sorbitol, polyvinylpyrrolidone, lecithin, polyethylene glycol, polysorbate, polyoxethylenestearate and dimethicon. 
     
     
         15 . The composition according to  claim 14 , wherein the composition comprises 20 to 60 mg orlistat. 
     
     
         16 . The composition according to  claim 15 , in the form of a tablet, a chewable tablet or capsule for oral administration.